Radiprodil-RGH-896-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERadiprodilCat. No.: HY-14777CAS No.: 496054-87-6Synonyms: RGH-896分式: CHFNO分量: 397.4作靶點: iGluR作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實

2、驗 DMSO : 250 mg/mL (629.09 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.5164 mL 12.5818 mL 25.1636 mL5 mM 0.5033 mL 2.5164 mL 5.0327 mL10 mM 0.2516 mL 1.2582 mL 2.5164 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添加助溶?為保證實驗結(jié)果的可

3、靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.23 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.23 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% cor

4、n oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (5.23 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Radiprodil (RGH-896)具有服活性的、NMDA 受體 NR2B 亞類的選擇性拮抗劑。 種可于治療神經(jīng)性疼痛和其它慢性疼痛的潛在藥物。IC50 & Target NMDA NR2B 1.體外研究 Preincubation with Radiprodil (10 nM) restores long-term potentiation

5、(LTP) in the presence of A1-42, 3NTyr10-A and A1-40, but not ApE3 2.As for LTP, Radiprodil (10 nM) reverses the synaptic toxicity of 3NTyr-AA1-40 and A1-42 but not that ApE3-42 2.體內(nèi)研究 Radiprodil could block NMDA currents in Mg2+ insensitive variants, with potencies similar to those obtainedwithout M

6、g2+ 3.Radiprodils potency is higher at pH 7.0 than at pH 7.6, suggesting that radiprodil may retain its ability toblock glutamate-induced NMDA currents even under acidic conditions that manifest under long term seizures3.REFERENCES1. Mony L, et al. Allosteric modulators of NR2B-containing NMDA recep

7、tors: molecular mechanisms and therapeutic potential. Br JPharmacol. 2009 Aug;157(8):1301-17.2. Rammes G, et al. The NMDA receptor antagonist Radiprodil reverses the synaptotoxic effects of different amyloid-beta (A) species onlong-term potentiation (LTP). Neuropharmacology. 2018 Sep 15;140:184-192.3. Mullier B, et al. GRIN2B gain of function mutations are sensitive to radiprodil, a negative allosteric modulator of GluN2B-containingNMDA receptors. Neuropharmacology. 2017 Sep 1;123:322-331.McePdfHeightCaution: Product has not been fully validated for medical applications.For